RU2007111467A - CONTRAST AGENT TARGETED AT THE PLASMINOGEN UROKINASE ACTIVATOR RECEPTOR - Google Patents

CONTRAST AGENT TARGETED AT THE PLASMINOGEN UROKINASE ACTIVATOR RECEPTOR Download PDF

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RU2007111467A
RU2007111467A RU2007111467/15A RU2007111467A RU2007111467A RU 2007111467 A RU2007111467 A RU 2007111467A RU 2007111467/15 A RU2007111467/15 A RU 2007111467/15A RU 2007111467 A RU2007111467 A RU 2007111467A RU 2007111467 A RU2007111467 A RU 2007111467A
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agent according
imaging
visualization agent
group
alanine
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RU2394837C2 (en
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Алан КАТБЕРТСОН (NO)
Алан КАТБЕРТСОН
Бенте Е. АРБО (NO)
Бенте Е. АРБО
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Джи-И Хелткер АС (NO)
Джи-И Хелткер АС
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10—Organic compounds
    • A61K49/14—Peptides, e.g. proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/005—Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
    • A61K49/0056—Peptides, proteins, polyamino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/10—Peptides having 12 to 20 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0032—Methine dyes, e.g. cyanine dyes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins

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  • Life Sciences & Earth Sciences (AREA)
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  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Radiology & Medical Imaging (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Magnetic Resonance Imaging Apparatus (AREA)
  • Ultra Sonic Daignosis Equipment (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Claims (18)

1. Агент визуализации рецептора урокиназного активатора плазминогена (uPAR) формулы Ia1. Agent urokinase plasminogen activator receptor imaging agent (uPAR) of formula Ia
Figure 00000001
Figure 00000001
 где Х0 представляет собой от 1 до 5 аминокислот,where X 0 represents from 1 to 5 amino acids, X1, Х2, Х3, Х4 и Х5 независимо представляют собой одну аминокислоту,X 1 , X 2 , X 3 , X 4 and X 5 independently represent one amino acid, Phe представляет собой фенилаланин,Phe is phenylalanine, Leu представляет собой лейцин,Leu is a leucine, Trp представляет собой триптофан,Trp is tryptophan, Х6 представляет собой от 0 до 5 аминокислот или определен формулой (Ib)X 6 represents from 0 to 5 amino acids or is defined by formula (Ib)
Figure 00000002
Figure 00000002
 где обозначения являются такими, как определено для формулы la,where the designations are as defined for formula la, и где β-Ala представляет собой β-аланин,and where β-Ala is β-alanine, Lys представляет собой лизин,Lys is lysine, β-Ala формулы Ib связан с Х5 формулы Ia, и гдеβ-Ala of formula Ib is linked to X 5 of formula Ia, and where W1 и W2 представляют собой одинаковые или разные группировки, и индивидуально представляют собой спейсер, биомодификатор или отсутствуют, и по меньшей мере присутствует один Z1 или Z2, представляющий собой визуализируемую группировку, способную к обнаружению либо непосредственно, либо косвенно в процессе диагностической визуализации.W 1 and W 2 represent the same or different groups, and individually represent a spacer, a biomodifier or are absent, and at least one Z 1 or Z 2 is present, which is a visualized group capable of detecting either directly or indirectly in the diagnostic process renderings. 2. Агент визуализации по п.1, где Х0 представляет собой от 1 до 5 аминокислот, выбранных из группы аланина, треонина, глицина, аспарагиновой кислоты и глутаминовой кислоты.2. The visualization agent according to claim 1, where X 0 represents from 1 to 5 amino acids selected from the group of alanine, threonine, glycine, aspartic acid and glutamic acid. 3. Агент визуализации по п.1, где X1 представляет собой β-циклоалкилаланин.3. The visualization agent according to claim 1, where X 1 represents β-cycloalkylalanine. 4. Агент визуализации по п.1, где Х2 представляет собой серин или аланин.4. The visualization agent according to claim 1, where X 2 represents serine or alanine. 5. Агент визуализации по п.1, где Х3 представляет собой аргинин, миметик аргинина, тирозин или аланин.5. The visualization agent according to claim 1, where X 3 is arginine, an arginine mimetic, tyrosine or alanine. 6. Агент визуализации по п.1, где Х4 представляет собой тирозин, аланин, лейцин или циклогексилаланин.6. The visualization agent according to claim 1, where X 4 is tyrosine, alanine, leucine or cyclohexylalanine. 7. Агент визуализации по п.1, где X5 представляет собой серин, гистидин, аланин, тирозин или лейцин.7. The imaging agent according to claim 1, where X 5 is serine, histidine, alanine, tyrosine or leucine. 8. Агент визуализации по п.1, где Х6 содержит аминокислоты, выбранные из группы глицина, аспарагиновой кислоты, лизина, фенилаланина или β-аланина, либо отсутствует.8. The visualization agent according to claim 1, where X 6 contains amino acids selected from the group of glycine, aspartic acid, lysine, phenylalanine or β-alanine, or is absent. 9. Агент визуализации по п.1, содержащий пептидную последовательность Z1-W1-X0-Cha-Phe-Ser-Arg-Tyr-Leu-Trp-Ser-X6-W2-Z2, где Cha представляет собой циклогексилаланин, Ser представляет собой серин, Arg представляет собой аргинин, Tyr представляет собой тирозин, а все остальные обозначения являются такими, как определено ранее.9. The visualization agent according to claim 1, containing the peptide sequence Z 1 -W 1 -X 0 -Cha-Phe-Ser-Arg-Tyr-Leu-Trp-Ser-X 6 -W 2 -Z 2 where Cha represents cyclohexylalanine, Ser is serine, Arg is arginine, Tyr is tyrosine, and all other symbols are as previously defined. 10. Агент визуализации по п.1, где по меньшей мере один из W1 и W2 содержит от 1 до 10 ед. монодисперсного полиэтиленгликолевого (ПЭГ) структурного элемента или от 1 до 10 аминокислотных остатков.10. The visualization agent according to claim 1, where at least one of W 1 and W 2 contains from 1 to 10 units. monodispersed polyethylene glycol (PEG) structural element or from 1 to 10 amino acid residues. 11. Агент визуализации по п.1, где один или оба Z1 и Z2 представляют собой визуализируемую группировку для использования в диагностике in vivo, содержащую группировку, обнаруживаемую при радио-, ОЭКТ - (однофотонная эмиссионная компьютерная томография), ПЭТ - (позитронная эмиссионная томография), рентгеновской, МР (магнитно-резонансной), ультразвуковой или оптической визуализации.11. The imaging agent according to claim 1, where one or both Z 1 and Z 2 represent a visualized group for use in in vivo diagnostics, containing a group detected by radio, SPECT - (single photon emission computed tomography), PET - (positron emission tomography), X-ray, MR (magnetic resonance), ultrasound or optical imaging. 12. Агент визуализации по п.11, где один или оба Z1 и Z2 содержат группировку М, представляющую собой гамма-излучающую группировку для радио- или ОЭКТ-визуализации, выбранную из 67Ga, 111In, 123I, 125I, 131I, 81mKr, 99Мо, 99mTc, 201Tl и 133Хе.12. The imaging agent according to claim 11, where one or both of Z 1 and Z 2 contain a moiety M, which is a gamma-emitting moiety for radio or SPECT imaging, selected from 67 Ga, 111 In, 123 I, 125 I, 131 I, 81m Kr, 99 Mo, 99m Tc, 201 Tl and 133 Xe. 13. Агент визуализации по п.11, где один или оба Z1 и Z2 содержат группировку М, представляющую собой радиоактивный излучатель со свойствами испускания позитронов для ПЭТ-визуализации, выбранную из 11С, 18F, 13N, 15O, 77F, 75Br, 76Br, 124I, 64Cu, 48V, 52Fe, 55Co, 94mTc, 68Ga или 82Rb.13. The visualization agent according to claim 11, where one or both Z 1 and Z 2 contain a group M, which is a radioactive emitter with the properties of emitting positrons for PET imaging, selected from 11 C, 18 F, 13 N, 15 O, 77 F, 75 Br, 76 Br, 124 I, 64 Cu, 48 V, 52 Fe, 55 Co, 94m Tc, 68 Ga or 82 Rb. 14. Агент визуализации по п.11, где один или оба Z1 и Z2 содержат группировку М, представляющую собой парамагнитный металл, выбранный из группы Gd(III), Mn(II), Cu(II), Cr(III), Fe(III), Co(II), Er(II), Ni(II), Eu(III) или Dy(III), либо оксид металла, такой как оксид металла суперпарамагнитного, ферримагнитного или ферромагнитного типа, для МР визуализации.14. The visualization agent according to claim 11, where one or both Z 1 and Z 2 contain a group M, which is a paramagnetic metal selected from the group Gd (III), Mn (II), Cu (II), Cr (III), Fe (III), Co (II), Er (II), Ni (II), Eu (III) or Dy (III), or a metal oxide, such as superparamagnetic, ferrimagnetic or ferromagnetic type metal oxide, for MR imaging. 15. Агент визуализации по п.11, где по меньшей мере любой из Z1 и Z2 представляет собой светорассеиватель, светопоглотитель или светоизлучатель для оптической визуализации.15. The imaging agent according to claim 11, where at least any of Z 1 and Z 2 is a diffuser, light absorber or light emitter for optical imaging. 16. Фармацевтическая композиция, содержащая агент визуализации по любому из пп.1-15 вместе с одним или более фармацевтически приемлемыми адъювантами, эксципиентами или разбавителями.16. A pharmaceutical composition comprising an imaging agent according to any one of claims 1 to 15, together with one or more pharmaceutically acceptable adjuvants, excipients or diluents. 17. Агент визуализации по любому из пп.1-15 для применения в диагностической визуализации.17. The imaging agent according to any one of claims 1 to 15 for use in diagnostic imaging. 18. Способ получения изображений организма человека или животного посредством диагностической визуализации, включающий введение в указанный организм агента визуализации по любому из пп.1-15 и получение изображения по меньшей мере части указанного организма, в который введен указанный агент визуализации.18. A method of obtaining images of the human or animal organism through diagnostic imaging, comprising introducing into the specified organism a visualization agent according to any one of claims 1 to 15 and obtaining an image of at least a portion of the specified organism into which the specified visualization agent is introduced.
RU2007111467/04A 2004-09-29 2005-09-28 Contrast agent aimed at urokinase plasminogen activator receptor RU2394837C2 (en)

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JP (1) JP5122962B2 (en)
KR (1) KR101248350B1 (en)
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AU (1) AU2005287934B2 (en)
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US20070190068A1 (en) * 2005-10-10 2007-08-16 Richard Hart uPAR-binding molecule-drug conjugates and uses thereof
JP2010513476A (en) * 2006-12-20 2010-04-30 ジーイー・ヘルスケア・アクスイェ・セルスカプ Contrast agent
GB0718967D0 (en) * 2007-09-28 2007-11-07 Ge Healthcare Ltd Peptide imaging agents
GB0718957D0 (en) * 2007-09-28 2007-11-07 Ge Healthcare Ltd Optical imaging agents
CN107362376A (en) * 2010-07-27 2017-11-21 通用电气健康护理有限公司 Radiopharmaceutical composition
WO2013167130A1 (en) * 2012-05-08 2013-11-14 Rigshospitalet 177-Lu LABELED PEPTIDE FOR SITE-SPECIFIC uPAR-TARGETING
WO2014086364A1 (en) 2012-12-03 2014-06-12 Rigshospitalet Positron emitting radionuclide labeled peptides for human upar pet imaging
ES2828954T3 (en) * 2014-09-17 2021-05-28 Fluoguide As UPAR Site-Specific Peptide for Use in Perioperative Optical Imaging of Invasive Cancer
US20210138090A1 (en) * 2014-09-17 2021-05-13 Fluoguide A/S uPAR targeting peptide for use in peroperative optical imaging of invasive cancer
PT3166606T (en) * 2015-06-03 2018-10-01 Surgimab S A S Fluorescent conjugates
EP3759121A1 (en) * 2018-03-01 2021-01-06 Trigemina, Inc. Labeled oxytocin and method of manufacture and use
JP2022544647A (en) * 2019-07-16 2022-10-20 リグスホスピタレット Urokinase plasminogen activator receptor targeting peptide
EP3999123A1 (en) * 2019-07-16 2022-05-25 Fluoguide A/S A receptor-targeting conjugate with an effective pharmacokinetic profile
KR20230173075A (en) 2020-12-01 2023-12-26 큐라사이트 에이/에스 Urokinase Plasminogen Activator Receptor Targeted Radiolabeled Peptide Conjugates
US20240066142A1 (en) * 2021-01-15 2024-02-29 Fluoguide A/S A upar (urokinase plasminogen activator receptor)-targeting conjugate

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AR020101A1 (en) * 1998-07-01 2002-04-10 Cancerforskingsfonden Af 1989 A PEPTIDE ANTAGONIST OF THE HUMAN UROQUINASE RECEPTOR, PHARMACEUTICAL COMPOSITION CONTAINING HIM, ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND METHODOPARA TO SELECT AN ADEQUATE PEPTIDE ANTAGONIST.
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ATE447417T1 (en) 2004-03-04 2009-11-15 Ge Healthcare As CONJUGATES OF ANGIOTENSIN-PEPTIDE ANALOGAS AND CHELATING AGENTS FOR DIAGNOSIS AND THERAPY

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CN101065152A (en) 2007-10-31
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WO2006036071A2 (en) 2006-04-06
KR20070083604A (en) 2007-08-24
US8568689B1 (en) 2013-10-29
BRPI0516168A (en) 2008-08-26
MX2007003750A (en) 2007-11-07
AU2005287934B2 (en) 2009-03-26
CA2580464A1 (en) 2006-04-06
AU2005287934A1 (en) 2006-04-06
KR101248350B1 (en) 2013-04-01
JP5122962B2 (en) 2013-01-16
WO2006036071A3 (en) 2007-02-15
JP2008514588A (en) 2008-05-08

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